NEW MATERIAL:Aminophenyl ether derivatives of formula I [R is H, halogen, alkyl; R1 is H, alkyl; R2 is cyclohexyl; R3 is H, alkyl, phenyl; R4 is H, alkyl, aryl; R5 is H, aryl, -COR6, -CH2R6 (R6 is H, alkyl, cyclohexyl, aryl): where R2 and R2 may incorporate to form cyclohexane; R4 and R5 may combine to form pyrrolidine or piperidine ring].
EXAMPLE: cis-1-[4-(P-menthane-8-yloxy)phenyl]piperidine.
USE: Anticholesteremic; they have activities of lowering cholesterol and triglyceride and increasing selectively high-density lipoprotein in blood.
PREPARATION: For example, the cis- or trans-isomer of an alcohol of formula II is reacted with a compound of formula III (X is halogen) in the presence of a strong base and the product is reduced to give the cis- or trans-isomer of the compound of formula I (R4, R5 are H).
KOJIMA ATSUO
OOHATA ISAO
SATOU NOBORU